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基于壳聚糖的接枝和交联共聚物对双氯芬酸钠药物(DS)的药物释放比较研究

Comparative Drug Release Investigations for Diclofenac Sodium Drug (DS) by Chitosan-Based Grafted and Crosslinked Copolymers.

作者信息

Chopra Lalita, Thakur Kamal Kishor, Chohan Jasgurpreet Singh, Sharma Shubham, Ilyas R A, Asyraf M R M, Zakaria S Z S

机构信息

Department of Chemistry, University Institute of Sciences (UIS), Chandigarh University, Gharuan, Mohali 140413, Punjab, India.

Mechanical Engineering Department, University Centre for Research & Development, Chandigarh University, Mohali 140413, Punjab, India.

出版信息

Materials (Basel). 2022 Mar 24;15(7):2404. doi: 10.3390/ma15072404.

Abstract

The hydrogels responding to pH synthesized by graft copolymerization only and then concurrent grafting and crosslinking of monomer N-isopropyl acrylamide (NIPAAM) and binary comonomers acrylamide, acrylic acid and acrylonitrile (AAm, AA and AN) onto chitosan support were explored for the percent upload and release study for anti-inflammatory diclofenac sodium drug (DS), w.r.t. time and pH. Diclofenac sodium DS was seized in polymeric matrices by the equilibration process. The crosslinked-graft copolymers showed the highest percent uptake than graft copolymers (without crosslinker) and chitosan itself. The sustainable release of the loaded drug was studied with respect to time at pH 2.2, 7.0, 7.4 and 9.4. Among graft copolymers (without crosslinking), Chit-g-polymer (NIPAAM-co-AA) and Chit-g-polymer (NIPAAM-co-AN) exhibited worthy results for sustainable drug deliverance, whereas Crosslink-Chit-g-polymer (NIPAAM-co-AA) and Crosslink-Chit-g-polymer (NIPAAM-co-AAm) presented the best results for controlled/sustained release of diclofenac sodium DS with 93.86 % and 96.30 % percent release, respectively, in 6 h contact time. Therefore, the grafted and the crosslinked graft copolymers of the chitosan showed excellent delivery devices for the DS with sustainable/prolonged release in response to pH. Drug release kinetics was studied using Fick’s law. The kinetic study revealed that polymeric matrices showed the value of n as n > 1.0, hence drug release took place by non-Fickian diffusion. Hence, the present novel findings showed the multidirectional drug release rate. The morphological changes due to interwoven network structure of the crosslinked are evident by the Scanning electron microscopy (SEM) analysis.

摘要

仅通过接枝共聚合成,然后将单体N-异丙基丙烯酰胺(NIPAAM)与二元共聚单体丙烯酰胺、丙烯酸和丙烯腈(AAm、AA和AN)同时接枝和交联到壳聚糖载体上,制备了对pH有响应的水凝胶,并针对抗炎药物双氯芬酸钠(DS)的载药量和释放量进行了时间和pH方面的研究。双氯芬酸钠DS通过平衡过程被捕获在聚合物基质中。交联接枝共聚物的摄取百分比高于接枝共聚物(无交联剂)和壳聚糖本身。在pH为2.2、7.0、7.4和9.4的条件下,研究了载药的持续释放情况。在接枝共聚物(无交联)中,壳聚糖-g-聚合物(NIPAAM-co-AA)和壳聚糖-g-聚合物(NIPAAM-co-AN)在药物持续递送方面表现出良好效果;而交联壳聚糖-g-聚合物(NIPAAM-co-AA)和交联壳聚糖-g-聚合物(NIPAAM-co-AAm)在双氯芬酸钠DS的控释/缓释方面表现最佳,在6小时接触时间内的释放百分比分别为93.86%和96.30%。因此,壳聚糖的接枝和交联接枝共聚物显示出优异的递送装置,可使DS在响应pH时实现持续/长效释放。使用菲克定律研究了药物释放动力学。动力学研究表明,聚合物基质的n值大于1.0,因此药物释放通过非菲克扩散发生。因此,目前的新发现显示了多向药物释放速率。通过扫描电子显微镜(SEM)分析可以明显看出交联导致的交织网络结构引起的形态变化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e07/9000032/5d896b79d675/materials-15-02404-g001.jpg

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